AZD4547 is a potent, selective and orally active pan-FGFR inhibitor with IC50s of 0.2. 2.5, 1.8 and 165 nM for FGFR1, 2, 3 and 4, respectively.
|Cell lines||MCF-7 cell line|
|Preparation method||In vitro cell-cycle and apoptotic induction analysis
Cell lines were incubated with fixed concentrations of AZD4547 for 72 hours. For fluorescence-activated cell sorting (FACS), cells were fixed with 70% ethanol and then incubated with propidium iodide/RNase A (Sigma) labeling solution. Cell-cycle profiles were assessed with a FACSCalibur instrument and CellQuest analysis software (Becton Dickinson). For apoptotic analysis, cells and media were gently harvested and centrifuged, followed by washing of cell pellets. Cells were then processed for Annexin V-fluorescein isothiocyanate (FITC) staining and propidium iodide uptake according to the manufacturer's instructions (Abcam). The proportion of cells staining positive for Annexin V were then assessed with a FACSCalibur instrument and quadrant sorting was done by CellQuest analysis software (Becton Dickinson).
|Incubation time||72 h|
|Animal models||nude mice bearing established Calu-6 human tumor xenografts|
|Formulation||formulated in a 1% (v/v) solution of polyoxyethylenesorbitan monooleate (Tween-80) in deionized water|
|Dosages||1.5–50 mg/kg once daily or twice daily|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
Tumour cell responses to new fibroblast growth factor receptor tyrosine kinase inhibitors and identification of a gatekeeper mutation in FGFR3 as a mechanism of acquired resistance.
Chell et al. Oncogene. 2012 Aug 6. PMID: 22869148.
AZD4547: an orally bioavailable, potent, and selective inhibitor of the fibroblast growth factor receptor tyrosine kinase family.
Gavine et al. Cancer Res. 2012 Apr 15;72(8):2045-56. PMID: 22369928.
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